Deciphering the detailed structure-activity relationship of coumarins as Monoamine oxidase enzyme inhibitors-An updated review

Chem Biol Drug Des. 2021 Oct;98(4):655-673. doi: 10.1111/cbdd.13919. Epub 2021 Jul 26.

Abstract

In the last few years, Monoamine oxidase (MAO) have emerged as a target for the treatment of many neurodegenerative diseases including anxiety, depression, Alzheimer's, and Parkinson's diseases. The MAO inhibitors especially selective and reversible inhibitors of either of the isoenzymes (MAO-A & MAO-B) have been given more attention as both the form have different therapeutic properties and hence can be used for different neurological disorders. The lack of selective and reversible inhibitors available for both the enzymes and severity of the neuronal disorder in society have opened a new door to the researchers to carry out large and dedicated researches in this field. Among the several classes of the molecule as the inhibitors, coumarins hold a rank as a potent scaffold with its ease of synthesis, high therapeutic potential, and reversibility in inhibiting MAOs. The current review is an update of the research in the field that covers the works during the last six years (2014-2020) with a major focus on the SAR of the coumarin derivatives including synthetic, natural, and hybrids of coumarins with FDA-approved drugs.

Keywords: Alzheimer's disease; coumarin; monoamine oxidase; structure-activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Cell Extracts / chemistry
  • Coumarins / chemical synthesis*
  • Coumarins / pharmacology
  • Fungi / chemistry
  • Humans
  • Molecular Structure
  • Monoamine Oxidase / metabolism*
  • Monoamine Oxidase Inhibitors / chemical synthesis*
  • Monoamine Oxidase Inhibitors / pharmacology
  • Neurodegenerative Diseases / drug therapy*
  • Protein Binding
  • Structure-Activity Relationship

Substances

  • Cell Extracts
  • Coumarins
  • Monoamine Oxidase Inhibitors
  • Monoamine Oxidase